Recent update on development of small-molecule STAT3 inhibitors for cancer therapy: from phosphorylation inhibition to protein degradation

J Dong, XD Cheng, WD Zhang… - Journal of Medicinal …, 2021 - ACS Publications
Signal transducer and activator of transcription 3 (STAT3) is a transcription factor that
regulates various biological processes, including proliferation, metastasis, angiogenesis …

Structural biology of STAT3 and its implications for anticancer therapies development

J Sgrignani, M Garofalo, M Matkovic, J Merulla… - International journal of …, 2018 - mdpi.com
Transcription factors are proteins able to bind DNA and induce the transcription of specific
genes. Consequently, they play a pivotal role in multiple cellular pathways and are …

Allosteric modulator discovery: from serendipity to structure-based design

S Lu, X He, D Ni, J Zhang - Journal of medicinal chemistry, 2019 - ACS Publications
Allosteric modulators bound to structurally diverse allosteric sites can achieve better
pharmacological advantages than orthosteric ligands. The discovery of allosteric …

Inhibiting STAT3 signaling pathway by natural products for cancer prevention and therapy: In vitro and in vivo activity and mechanisms of action

J Yang, L Wang, X Guan, JJ Qin - Pharmacological Research, 2022 - Elsevier
Signal transducer and activator of transcription 3 (STAT3) plays a critical role in signal
transmission from the plasma membrane to the nucleus, regulating the expression of genes …

Revisiting signal transducer and activator of transcription 3 (STAT3) as an anticancer target and its inhibitor discovery: Where are we and where should we go?

Q Huang, Y Zhong, H Dong, Q Zheng, S Shi… - European Journal of …, 2020 - Elsevier
As a transcription factor, STAT3 protein transduces extracellular signals to the nucleus and
then activates transcription of target genes. STAT3 has been well validated as an attractive …

Discovery of STAT3 and histone deacetylase (HDAC) dual-pathway inhibitors for the treatment of solid cancer

Y Ren, S Li, R Zhu, C Wan, D Song, J Zhu… - Journal of Medicinal …, 2021 - ACS Publications
Nowadays, simultaneous inhibition of multiple targets through drug combination is an
important anticancer strategy owing to the complex mechanism behind tumorigenesis …

Ginsenoside Rd ameliorates muscle wasting by suppressing the signal transducer and activator of transcription 3 pathway

YT Wijaya, T Setiawan, IN Sari, K Park… - Journal of cachexia …, 2022 - Wiley Online Library
Background The effects of some drugs, aging, cancers, and other diseases can cause
muscle wasting. Currently, there are no effective drugs for treating muscle wasting. In this …

In silico structure-based approaches to discover protein-protein interaction-targeting drugs

WH Shin, CW Christoffer, D Kihara - Methods, 2017 - Elsevier
A core concept behind modern drug discovery is finding a small molecule that modulates a
function of a target protein. This concept has been successfully applied since the mid-1970s …

Napabucasin and related heterocycle-fused naphthoquinones as STAT3 inhibitors with antiproliferative activity against cancer cells

H Löcken, C Clamor, K Müller - Journal of natural products, 2018 - ACS Publications
Napabucasin (6) and its angularly anellated isomer (7), for which the synthesis is described,
together with related plant-derived naphthoquinones, were evaluated in vitro against human …

Discovery, Optimization, and Evaluation of Novel N-(Benzimidazol-5-yl)-1,3,4-thiadiazol-2-amine Analogues as Potent STAT3 Inhibitors for Cancer Treatment

R Wang, TT Du, WQ Liu, YC Liu, YD Yang… - Journal of Medicinal …, 2023 - ACS Publications
Signal transducer and activator of transcription 3 (STAT3) is an attractive target for cancer
therapy. However, identifying potent and selective STAT3 small-molecule inhibitors with …